申请人:SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.
公开号:US10039775B2
公开(公告)日:2018-08-07
Disclosed is a preparation method for an antitumor drug AP26113 (I). The method comprises the following preparation steps: cyclizing N-[2-methoxyl-4[4-(dimethyl amino)piperid-1-yl]aniline]guanidine and N,N-dimethylamino acrylate, condensing N-[2-methoxyl-4[4-(dimethyl amino)piperid-1-yl]aniline]guanidine and 4-(dimethyl phosphitylate)aniline, and chlorinating N-[2-methoxyl-4[4-(dimethyl amino)piperid-1-yl]aniline]guanidine and a chlorinating agent, sequentially, so as to prepare AP26113 (I). The preparation method adopts easily-obtained raw materials, causes few side reactions, and is economical, environmentally friendly, and suitable for industrial production.
揭示了一种抗肿瘤药物AP26113(I)的制备方法。该方法包括以下制备步骤:环化N-[2-甲氧基-4-[4-(二甲基氨基)哌啶-1-基]苯胍]和N,N-二甲基丙烯酰胺,缩合N-[2-甲氧基-4-[4-(二甲基氨基)哌啶-1-基]苯胍]和4-(二甲基磷酰基)苯胺,以及氯化N-[2-甲氧基-4-[4-(二甲基氨基)哌啶-1-基]苯胍]和氯化剂,依次制备AP26113(I)。该制备方法采用易得的原料,引起少量副反应,经济、环保,适合工业生产。